ML204

Modify Date: 2024-01-12 12:46:43

ML204 Structure
ML204 structure
Common Name ML204
CAS Number 5465-86-1 Molecular Weight 226.317
Density 1.1±0.1 g/cm3 Boiling Point 404.4±33.0 °C at 760 mmHg
Molecular Formula C15H18N2 Melting Point N/A
MSDS Chinese USA Flash Point 198.4±25.4 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of ML204


ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.IC50 value:Target: TRPC4/C5 inhibitorML204 inhibited TRPC4β-mediated intracellular Ca(2+) rise with an IC(50) value of 0.96 μm and exhibited 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation. In whole-cell patch clamp recordings, ML204 blocked TRPC4β currents activated through either μ-opioid receptor stimulation or intracellular dialysis of guanosine 5'-3-O-(thio)triphosphate (GTPγS), suggesting a direct interaction of ML204 with TRPC4 channels rather than any interference with the signal transduction pathways. Selectivity studies showed no appreciable block by 10-20 μm ML204 of TRPV1, TRPV3, TRPA1, and TRPM8, as well as KCNQ2 and native voltage-gated sodium, potassium, and calcium channels in mouse dorsal root ganglion neurons. In isolated guinea pig ileal myocytes, ML204 blocked muscarinic cation currents activated by bath application of carbachol or intracellular infusion of GTPγS, demonstrating its effectiveness on native TRPC4 currents [1]. ML204 blocked TRPC4 channels in an electrophysiological assay with an IC value of 2.6 μM and was also active in fluorescent and electrophysiological assays in which TRPC4 channels were activated by different mechanisms, indicating direct block of TRPC4 channels. Selectivity for block of TRPC4 channels was examined in fluorescent and electrophysiological experiments against closely related TRPC channels and more distantly related TRPV, TRPA and TRPM channels, and against non-TRP ion channels. ML204 afforded good selectivity (19-fold) against TRPC6 channels and more modest selectivity against TRPC3 and TRPC5 (9-fold) channels [2].

 Names

Name 4-methyl-2-piperidin-1-ylquinoline
Synonym More Synonyms

 ML204 Biological Activity

Description ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.IC50 value:Target: TRPC4/C5 inhibitorML204 inhibited TRPC4β-mediated intracellular Ca(2+) rise with an IC(50) value of 0.96 μm and exhibited 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation. In whole-cell patch clamp recordings, ML204 blocked TRPC4β currents activated through either μ-opioid receptor stimulation or intracellular dialysis of guanosine 5'-3-O-(thio)triphosphate (GTPγS), suggesting a direct interaction of ML204 with TRPC4 channels rather than any interference with the signal transduction pathways. Selectivity studies showed no appreciable block by 10-20 μm ML204 of TRPV1, TRPV3, TRPA1, and TRPM8, as well as KCNQ2 and native voltage-gated sodium, potassium, and calcium channels in mouse dorsal root ganglion neurons. In isolated guinea pig ileal myocytes, ML204 blocked muscarinic cation currents activated by bath application of carbachol or intracellular infusion of GTPγS, demonstrating its effectiveness on native TRPC4 currents [1]. ML204 blocked TRPC4 channels in an electrophysiological assay with an IC value of 2.6 μM and was also active in fluorescent and electrophysiological assays in which TRPC4 channels were activated by different mechanisms, indicating direct block of TRPC4 channels. Selectivity for block of TRPC4 channels was examined in fluorescent and electrophysiological experiments against closely related TRPC channels and more distantly related TRPV, TRPA and TRPM channels, and against non-TRP ion channels. ML204 afforded good selectivity (19-fold) against TRPC6 channels and more modest selectivity against TRPC3 and TRPC5 (9-fold) channels [2].
Related Catalog
References

[1]. Miller M, et al. Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. J Biol Chem. 2011 Sep 23;286(38):33436-46.

[2]. Miller MR, et al. Novel Chemical Inhibitor of TRPC4 Channels. Probe Reports from the NIH Molecular Libraries Program [Internet].

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 404.4±33.0 °C at 760 mmHg
Molecular Formula C15H18N2
Molecular Weight 226.317
Flash Point 198.4±25.4 °C
Exact Mass 226.147003
PSA 16.13000
LogP 3.92
Vapour Pressure 0.0±0.9 mmHg at 25°C
Index of Refraction 1.617
Storage condition -20℃

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
RIDADR NONH for all modes of transport

 Synthetic Route

~89%

ML204 Structure

ML204

CAS#:5465-86-1

Literature: Kidwai; Sapra; Dave Synthetic Communications, 2000 , vol. 30, # 24 p. 4479 - 4488

~%

ML204 Structure

ML204

CAS#:5465-86-1

Literature: Kobayashi, Kazuhiro; Yoneda, Keiichi; Miyamoto, Kazuna; Morikawa, Osamu; Konishi, Hisatoshi Tetrahedron, 2004 , vol. 60, # 50 p. 11639 - 11645

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 Synonyms

Quinoline, 4-methyl-2-(1-piperidinyl)-
4-methyl-2-piperidylquinoline
4-methyl-2-(piperidin-1-yl)quinoline
2-Piperidino-4-methyl-chinolin
ML204
4-Methyl-2-(1-piperidinyl)-quinoline
4-Methyl-2-(1-piperidinyl)quinoline
2-Piperidino-lepidin
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